PEG Conjugate Drug with Urea Carbonyl Linker for Multi-Drug Loading
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Solution Overview
Problem
Current PEGylated drugs are limited to monodrugs, lacking flexibility in drug loading and adjustment of drug positions and types, which restricts their therapeutic efficacy and versatility in treating complex diseases like cancer.
Innovation Solution
The development of polyethylene glycol conjugated drugs with specific linking groups such as urea carbonyl and succinyl, allowing for increased drug loading and flexible adjustment of drug positions and types, enabling dual- or multi-dose configurations to enhance therapeutic effectiveness.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If PEGylated monodrugs are used, then the drug can stay in blood circulation longer and reduce renal elimination, but the drug loading capacity and flexibility in adjusting drug positions and types are limited
Solution Approach 1:
The patent divides the PEG carrier into multiple functional segments: a hydrophobic core region for drug loading, a linking region for attachment, and a PEG chain for circulation extension. This segmentation allows multiple drugs to be loaded at different positions while maintaining the circulation benefits of PEGylation
Solution Approach 2:
The PEG conjugate structure serves multiple functions simultaneously: it extends circulation time through its hydrophilic PEG chains, provides drug loading capacity through the hydrophobic core, and enables flexibility through adjustable linking regions that can accommodate different drug types and positions
2Reliability
If multiple drugs are grafted onto PEG, then therapeutic efficacy is enhanced through different biological pathways, but the complexity of drug composition and structure increases
Solution Approach 1:
The patent merges multiple drugs onto a single PEG carrier molecule, creating a unified conjugate structure that delivers multiple therapeutic agents simultaneously. This combining approach enhances therapeutic efficacy through multiple biological pathways while managing complexity through a standardized conjugate platform
3Quantity of substance
If drug loading is increased on PEG carriers, then more drugs can be delivered to target sites, but the solubility and stability of the conjugate may be affected
Solution Approach 1:
The patent creates distinct local regions within the PEG conjugate: a hydrophobic core region that accommodates high drug loading, a linking region that provides stable attachment, and hydrophilic PEG chains that maintain overall solubility and stability. This local quality differentiation allows high drug loading without compromising conjugate stability
Data Source
AI summary
The disclosure relates to the technical field of medicine, specifically to a polyethylene glycol conjugated drug, a preparation method therefor and use thereof, and relates in particular to a polyethylene glycol conjugated drug represented by formula (I) or a pharmaceutically acceptable salt thereof. The disclosure further relates to a method for preparation of the polyethylene glycol conjugated drug or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the polyethylene glycol conjugated drug or a pharmaceutically acceptable salt thereof, and use of the polyethylene glycol conjugated drug or a pharmaceutically acceptable salt thereof in preparation of a medicament.